Growth Control and Differentiation Program, Trescowthick Research Laboratories, Peter MacCallum Cancer Centre, Melbourne, Victoria, Australia.
Oncogene. 2012 Apr 12;31(15):1949-62. doi: 10.1038/onc.2011.394. Epub 2011 Sep 12.
The phosphatidylinositol 3-kinase (PI3K)/AKT and RAS oncogenic signalling modules are frequently mutated in sporadic human cancer. Although each of these pathways has been shown to play critical roles in driving tumour growth and proliferation, their activation in normal human cells can also promote cell senescence. Although the mechanisms mediating RAS-induced senescence have been well characterised, those controlling PI3K/AKT-induced senescence are poorly understood. Here we show that PI3K/AKT pathway activation in response to phosphatase and tensin homolog (PTEN) knockdown, mutant PI3K, catalytic, α polypeptide (PIK3CA) or activated AKT expression, promotes accumulation of p53 and p21, increases cell size and induces senescence-associated β-galactosidase activity. We demonstrate that AKT-induced senescence is p53-dependent and is characterised by mTORC1-dependent regulation of p53 translation and stabilisation of p53 protein following nucleolar localisation and inactivation of MDM2. The underlying mechanisms of RAS and AKT-induced senescence appear to be distinct, demonstrating that different mediators of senescence may be deregulated during transformation by specific oncogenes. Unlike RAS, AKT promotes rapid proliferative arrest in the absence of a hyperproliferative phase or DNA damage, indicating that inactivation of the senescence response is critical at the early stages of PI3K/AKT-driven tumourigenesis. Furthermore, our data imply that chronic activation of AKT signalling provides selective pressure for the loss of p53 function, consistent with observations that PTEN or PIK3CA mutations are significantly associated with p53 mutation in a number of human tumour types. Importantly, the demonstration that mTORC1 is an essential mediator of AKT-induced senescence raises the possibility that targeting mTORC1 in tumours with activated PI3K/AKT signalling may exert unexpected detrimental effects due to inactivation of a senescence brake on potential cancer-initiating cells.
磷脂酰肌醇 3-激酶 (PI3K)/AKT 和 RAS 致癌信号模块在散发性人类癌症中经常发生突变。尽管这些途径中的每一种都被证明在驱动肿瘤生长和增殖方面发挥着关键作用,但它们在正常人类细胞中的激活也可以促进细胞衰老。虽然已经很好地描述了介导 RAS 诱导衰老的机制,但控制 PI3K/AKT 诱导衰老的机制了解甚少。在这里,我们表明,PI3K/AKT 通路的激活是对磷酸酶和张力蛋白同源物 (PTEN) 敲低、突变 PI3K、催化、α 多肽 (PIK3CA) 或激活 AKT 表达的反应,促进 p53 和 p21 的积累,增加细胞大小并诱导衰老相关的 β-半乳糖苷酶活性。我们证明 AKT 诱导的衰老依赖于 p53,其特征是 mTORC1 依赖性调节 p53 翻译,以及 p53 蛋白在核仁定位和 MDM2 失活后稳定性增加。RAS 和 AKT 诱导衰老的潜在机制似乎不同,表明在特定癌基因的转化过程中,不同的衰老介质可能被解除调节。与 RAS 不同,AKT 在没有过度增殖阶段或 DNA 损伤的情况下促进快速增殖停滞,这表明在 PI3K/AKT 驱动的肿瘤发生的早期阶段,衰老反应的失活是至关重要的。此外,我们的数据表明 AKT 信号的慢性激活为 p53 功能丧失提供了选择性压力,这与在许多人类肿瘤类型中观察到的 PTEN 或 PIK3CA 突变与 p53 突变显著相关的结果一致。重要的是,证明 mTORC1 是 AKT 诱导衰老的必需介质,这增加了这样一种可能性,即在激活 PI3K/AKT 信号的肿瘤中靶向 mTORC1 可能会由于对潜在的癌症起始细胞的衰老制动的失活而产生意想不到的有害影响。